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Preparation, Characterization and Evaluation of Quetiapine Fumarate Solid Lipid Nanoparticles to Improve the Oral Bioavailability.

Narala A, Veerabrahma K - J Pharm (Cairo) (2013)

Bottom Line: The physical stability of optimized formulation F3 was checked at room temperature for 2 months.The relative bioavailability of quetiapine fumarate from optimized SLN preparation was increased by 3.71 times when compared with the reference quetiapine fumarate suspension.The obtained results are indicative of SLNs as potential lipid carriers for improving the bioavailability of quetiapine fumarate by minimizing first-pass metabolism.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmaceutics, University College of Pharmaceutical Sciences, Kakatiya University, Warangal, Andhra Pradesh 506009, India.

ABSTRACT
Quetiapine fumarate is an antipsychotic drug with poor oral bioavailability (9%) due to first-pass metabolism. Present work is an attempt to improve oral bioavailability of quetiapine fumarate by incorporating in solid lipid nanoparticles (SLN). Six quetiapine fumarate SLN formulations were developed using three different lipids by hot homogenisation followed by ultrasonication. The drug excipient compatibility was studied by differential scanning calorimetry (DSC). Stable quetiapine fumarate SLNs having a mean particle size of 200-250 nm with entrapment efficiency varying in between 80% and 92% were developed. The physical stability of optimized formulation F3 was checked at room temperature for 2 months. Comparative bioavailability studies were conducted in male Wistar rats after oral administration of quetiapine fumarate suspension and SLN formulation. The relative bioavailability of quetiapine fumarate from optimized SLN preparation was increased by 3.71 times when compared with the reference quetiapine fumarate suspension. The obtained results are indicative of SLNs as potential lipid carriers for improving the bioavailability of quetiapine fumarate by minimizing first-pass metabolism.

No MeSH data available.


Serum concentration versus time profile of quetiapine fumarate upon oral administration of SLN preparation (F3) and suspension (F7) in rats.
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fig4: Serum concentration versus time profile of quetiapine fumarate upon oral administration of SLN preparation (F3) and suspension (F7) in rats.

Mentions: The drug in the serum samples was estimated by using HPLC method [16]. Various pharmacokinetic parameters obtained for both suspension and SLN preparation following oral administration are given in Table 4. With SLN dispersion, the average peak plasma concentration of quetiapine fumarate is 1.902 ± 0.054 μg/mL, whereas in the case of suspension, the peak plasma concentration is 0.107 ± 0.004 μg/mL. The tmax is same for both suspension and SLN. The plasma concentration-time profiles of suspension and SLN formulation are shown in Figure 4. F3 profile is superior to that of suspension.


Preparation, Characterization and Evaluation of Quetiapine Fumarate Solid Lipid Nanoparticles to Improve the Oral Bioavailability.

Narala A, Veerabrahma K - J Pharm (Cairo) (2013)

Serum concentration versus time profile of quetiapine fumarate upon oral administration of SLN preparation (F3) and suspension (F7) in rats.
© Copyright Policy - open-access
Related In: Results  -  Collection

Show All Figures
getmorefigures.php?uid=PMC4590790&req=5

fig4: Serum concentration versus time profile of quetiapine fumarate upon oral administration of SLN preparation (F3) and suspension (F7) in rats.
Mentions: The drug in the serum samples was estimated by using HPLC method [16]. Various pharmacokinetic parameters obtained for both suspension and SLN preparation following oral administration are given in Table 4. With SLN dispersion, the average peak plasma concentration of quetiapine fumarate is 1.902 ± 0.054 μg/mL, whereas in the case of suspension, the peak plasma concentration is 0.107 ± 0.004 μg/mL. The tmax is same for both suspension and SLN. The plasma concentration-time profiles of suspension and SLN formulation are shown in Figure 4. F3 profile is superior to that of suspension.

Bottom Line: The physical stability of optimized formulation F3 was checked at room temperature for 2 months.The relative bioavailability of quetiapine fumarate from optimized SLN preparation was increased by 3.71 times when compared with the reference quetiapine fumarate suspension.The obtained results are indicative of SLNs as potential lipid carriers for improving the bioavailability of quetiapine fumarate by minimizing first-pass metabolism.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmaceutics, University College of Pharmaceutical Sciences, Kakatiya University, Warangal, Andhra Pradesh 506009, India.

ABSTRACT
Quetiapine fumarate is an antipsychotic drug with poor oral bioavailability (9%) due to first-pass metabolism. Present work is an attempt to improve oral bioavailability of quetiapine fumarate by incorporating in solid lipid nanoparticles (SLN). Six quetiapine fumarate SLN formulations were developed using three different lipids by hot homogenisation followed by ultrasonication. The drug excipient compatibility was studied by differential scanning calorimetry (DSC). Stable quetiapine fumarate SLNs having a mean particle size of 200-250 nm with entrapment efficiency varying in between 80% and 92% were developed. The physical stability of optimized formulation F3 was checked at room temperature for 2 months. Comparative bioavailability studies were conducted in male Wistar rats after oral administration of quetiapine fumarate suspension and SLN formulation. The relative bioavailability of quetiapine fumarate from optimized SLN preparation was increased by 3.71 times when compared with the reference quetiapine fumarate suspension. The obtained results are indicative of SLNs as potential lipid carriers for improving the bioavailability of quetiapine fumarate by minimizing first-pass metabolism.

No MeSH data available.